Article Text

PDF
Ocular hypotensive efficacy, safety and systemic absorption of AR-12286 ophthalmic solution in normal volunteers
  1. Casey Kopczynski1,2,
  2. Gary D Novack3,
  3. Dennis Swearingen4,
  4. Thomas van Haarlem1,2
  1. 1Department of R&D, Aerie Pharmaceuticals, Inc., Bridgewater, New Jersey, USA
  2. 2Department of R&D, Aerie Pharmaceuticals, Inc., Research Triangle Park, North Carolina, USA
  3. 3PharmaLogic Development, Inc., San Rafael, California, USA
  4. 4Celerion, Tempe, Arizona, USA
  1. Correspondence to Gary D Novack, PharmaLogic Development, Inc., 17 Bridgegate Drive, San Rafael CA 94903, USA; gary_novack{at}pharmalogic.com

Abstract

Background/aims To evaluate the ocular hypotensive efficacy, ocular and systemic safety, and systemic exposure of two formulations of 0.5% AR-12286 Ophthalmic Solution.

Methods This was a double-masked, single-centre, crossover study in 18 normal adult volunteers. Volunteers were randomised to one of two dosing sequences: Formulation A once daily, both eyes (OU) for 8 days, a 7-day minimum washout, and then Formulation B, or the reverse. The main outcome measures were ocular tolerability, intraocular pressure (IOP) and blood levels of AR-12286 and its metabolites.

Results Systemic absorption was low, with a majority of subjects showing no measurable drug concentration in plasma (<1 ng/ml) at any time point with either formulation. The most frequent ocular adverse events were conjunctival hyperaemia, eye irritation, instillation site reaction, increased lacrimation, and blurred vision which were relatively short-lived and judged as not clinically significant. Both formulations of AR-12286 produced substantial reductions from baseline IOP ranging from 3 to 7 mm Hg (p<0.0001).

Conclusions No differences were noted in ocular safety between formulations of AR-12286 0.5%, dosed once daily in the morning for 8 days. AR-12286 produced little systemic exposure to the parent compound or two known metabolites. Clinically and statistically significant reductions in IOP were seen in these normotensive subjects.

  • Glaucoma
  • Intraocular pressure
  • Pharmacology

Statistics from Altmetric.com

Request permissions

If you wish to reuse any or all of this article please use the link below which will take you to the Copyright Clearance Center’s RightsLink service. You will be able to get a quick price and instant permission to reuse the content in many different ways.